Fetkovska N, Pletscher A, Ferracin F, Amstein R, Buhler F R
Clinic of Pharmacotherapy, Medical Bionics Research Institute, Bratislava, Czechoslovakia.
Cardiovasc Drugs Ther. 1990 Jan;4 Suppl 1:105-9. doi: 10.1007/BF00053439.
Serotonin (5-hydroxytryptamine; 5HT) kinetics and platelet activation by 5HT were studied in patients with essential hypertension (n = 45), and in matched normotensive subjects (n = 45). Platelet response to 5HT and plasma beta-thromboglobulin increased with age in men, both normotensives and hypertensives. Beta-thromboglobulin and 5-hydroxyindoleacetic acid (5HIAA) excretion were higher in hypertensive men than in women. In women, no changes in platelet activity or 5HIAA excretion were found. 5HT plasma concentrations increased with blood pressure. Platelet 5HT uptake (Vmax and KM) were the lowest in hypertensive men greater than or equal to 60 years of age. This may indicate that 5HT uptake in vivo in normotensives is far below maximum (VNT much less than Vmax), whereas in hypertensive men it may be close to maximum (VHT approximately Vmax). This could reflect significantly higher 5HT plasma concentrations in vivo hypertensives than in normotensives. The reduced uptake (which was found only in hypertensive men) may indicate an insufficient compensation of the enhanced 5HT release from aggregating platelets in older men, in whom platelet activity is enhanced in vivo. It is concluded that the defect in platelet 5HT uptake in hypertensives--along with the enhanced platelet aggregation--may contribute to a critical increase in 5HT plasma concentrations locally. An increase in 5HT concentrations leads to biochemical changes (higher 5HIAA excretion) as well as to an enhanced stimulation by 5HT. This may be of clinical relevance especially in older men, in whom 5HT2-receptor mediated responses are enhanced.
在45例原发性高血压患者和45例年龄匹配的血压正常受试者中,研究了血清素(5 - 羟色胺;5HT)动力学以及5HT对血小板的激活作用。男性(包括血压正常者和高血压患者)中,血小板对5HT的反应以及血浆β - 血小板球蛋白水平随年龄增长而升高。高血压男性的β - 血小板球蛋白和5 - 羟吲哚乙酸(5HIAA)排泄量高于女性。在女性中,未发现血小板活性或5HIAA排泄有变化。5HT血浆浓度随血压升高而增加。年龄大于或等于60岁的高血压男性血小板5HT摄取量(Vmax和KM)最低。这可能表明,血压正常者体内5HT摄取远低于最大值(VNT远小于Vmax),而高血压男性体内的摄取可能接近最大值(VHT约等于Vmax)。这可能反映出高血压患者体内5HT血浆浓度显著高于血压正常者。摄取减少(仅在高血压男性中发现)可能表明老年男性中,聚集血小板释放的5HT增加,但未得到充分代偿,而这些男性体内血小板活性增强。研究得出结论,高血压患者血小板5HT摄取缺陷——以及血小板聚集增强——可能导致局部5HT血浆浓度急剧升高。5HT浓度升高会导致生化变化(5HIAA排泄增加)以及5HT刺激增强。这可能具有临床意义,尤其是在老年男性中,他们的5HT2受体介导的反应增强。